| Literature DB >> 11073664 |
E A Garrard1, E C Borman, B N Cook, E J Pike, D G Alberg.
Abstract
Trypanothione reductase (TR) catalyzes the NAPDH-dependent reduction of the spermidine-glutathione conjugate trypanothione, an antioxidant found in Trypanosomatid parasites. TR plays an essential role in the parasite's defense against oxidative stress and has emerged as a prime target for drug development. Here we report the synthesis of several trypanothione analogues and their inhibitory effects on T. cruzi TR. All are competitive inhibitors with K(i) values ranging from 30 to 91 microM.Entities:
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Year: 2000 PMID： 11073664 DOI： 10.1021/ol0065423
Source DB: PubMed Journal: Org Lett ISSN： 1523-7052 Impact factor: 6.005